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Oily injection containing doxycycline hydrochloride/poloxamer drug-loading particles

A technology of doxycycline hydrochloride and drug-loaded particles, which can be used in the fields of tetracycline active ingredients, pharmaceutical formulations, aerosol delivery, etc., and can solve problems such as difficult injections and increased viscosity of preparations

Active Publication Date: 2014-04-09
中农华威制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The in situ gelling injection containing P407 disclosed in the literature and patents uses water as the main solvent, and the concentration of P407 in the preparation must reach more than 20% to have a better sustained release effect; a certain amount of methyl alcohol is added to the preparation Blocking agents such as cellulose, sodium carboxymethylcellulose, highly substituted hydroxypropylcellulose (H-HPC) or hydroxypropylmethylcellulose (HPMC) can enhance the sustained release effect, but will cause the viscosity of the formulation to increase high, making injections more difficult

Method used

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  • Oily injection containing doxycycline hydrochloride/poloxamer drug-loading particles

Examples

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Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1, preparation 15% doxycycline hydrochloride injection

[0026] Preparation composition: doxycycline hydrochloride 150g, P407 100g, BHT0.2g, BHA0.1g, IPM added to 1 liter.

[0027] Preparation method: (1) Melt P407 at 65-75°C, then add doxycycline hydrochloride and 2-3 times the amount of methanol equivalent to doxycycline, stir well, distill under reduced pressure, remove methanol, and obtain a solid solution , crush the solid solution, and pass through a 40-mesh sieve to obtain doxycycline hydrochloride / P407 drug-loaded microparticles. (2) Disperse the drug-loaded particles in an appropriate amount of IPM, grind them to a particle size of about 100 μm with a colloid mill, and further grind them to a particle size of less than 10 μm with a sand mill, then add the remaining ingredients, and use a high-shear homogenizer at 5000 rpm 15% doxycycline hydrochloride injection was prepared after multiple times of homogenization under the same conditions.

Embodiment 2

[0028] Embodiment 2, preparation 10% doxycycline hydrochloride injection

[0029] Preparation composition: each liter contains 100 g of doxycycline hydrochloride, 50 g of P407, 30 g of HPMC, 0.2 g of BHT, 0.1 g of BHA, and 0.1 g of PG, and soybean oil for injection is added to the final volume.

[0030]Preparation method: (1) Melt P407 at 65-75°C, then add doxycycline hydrochloride and HPMC, mix well, add methanol equivalent to twice the amount of doxycycline, stir well, distill under reduced pressure, remove methanol to obtain a solid solution, which is pulverized and passed through a 40-mesh sieve to obtain drug-loaded particles containing doxycycline hydrochloride. (2) Disperse the drug-loaded particles in an appropriate amount of soybean oil, grind them to a particle size of about 100 μm with a colloid mill, and further grind them to a particle size of less than 8 μm with a sand mill, then add the remaining ingredients, and use a high-shear homogenizer to After repeated h...

Embodiment 3

[0031] Embodiment 3, preparation 8% doxycycline hydrochloride injection

[0032] Preparation composition: doxycycline hydrochloride 80g, P40780g, BHT0.2g, BHA0.1g, PG0.1g, corn oil for injection is added to 1 liter.

[0033] Preparation method: (1) Melt P407 at 65-75°C, then add doxycycline hydrochloride and methanol equivalent to twice the amount of doxycycline, stir well, cool and reduce pressure, remove methanol, and obtain a solid solution, The solid solution is pulverized and passed through a 40-mesh sieve to obtain doxycycline hydrochloride / P407 drug-loaded microparticles. (2) Disperse the drug-loaded particles in an appropriate amount of corn oil, grind them to a particle size of about 100 μm with a colloid mill, and further grind them to a particle size of less than 8 μm with a sand mill, then add the remaining ingredients, and use a high-shear homogenizer to 8% doxycycline hydrochloride injection was prepared after multiple times of homogenization under the condition...

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Abstract

The invention discloses an oily long-acting injection containing doxycycline hydrochloride / poloxamer 407 drug-loading particles, which is prepared by combining the doxycycline hydrochloride with poloxamer 407 into drug-loading particles and further dispersing the drug-loading particles into an oily medium and grinding. Hydroxypropyl methyl cellulose or high-substituted hydroxypropyl cellulose also can be added into the drug-loading particles, and the sustained-release effect of the preparation is obviously enhanced. The preparation process of the injection is simple, the drug release is uniform, the biocompatibility is good, irreversible damage to the tissue of the injection part is avoided, and the adopted sustained-release carrier can be degraded and excreted.

Description

technical field [0001] The invention belongs to the preparation technology of veterinary drug preparations, and specifically relates to preparing doxycycline hydrochloride and poloxamer 407 into drug-loaded particles, suspending the drug-loaded particles in an oily medium, and preparing doxycycline hydrochloride-containing drug-loaded particles for veterinary use Long-acting injections. Background technique [0002] The currently commercialized veterinary doxycycline injections and patented technologies are mostly in the form of solutions, and the preparations need to be stored with nitrogen, and the water, organic solvents, co-solvents, complexing agents, antioxidants, etc. The dosage of the auxiliary agent and the pH value of the preparation are very strict. If there is a slight deviation, the stability of the preparation will be problematic. This dosage form is not easy to prepare a stable high-concentration preparation, and the slow-release effect is not obvious. This do...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K9/06A61K31/65A61K47/44A61K47/34A61K47/38A61K47/12A61K47/10A61K47/14
Inventor 王玉万戴晓曦潘贞德翁志飞任雅楠沈力
Owner 中农华威制药股份有限公司
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